The present disclosure generally relates to development of water dispersible policosanol-cyclodextrin complexes for use in nutritional supplements and functional foods.
Cyclodextrins (sometimes abbreviated herein as “CD” or “CD's”) are cyclic oligosaccharides composed of 6, 7, or 8 α-(1-4)-linked anhydroglucose units. The α-, β-, and γ-cyclodextrins prepared from starch are considered natural and are GRAS according to the USFDA. The cyclodextrins are widely used in the pharmaceutical industry to improve dissolution, stability and uptake of lipophilic molecules.
Policosanol is a complex mixture of lipophilic very long-chain alcohols (C24-C34) isolated from waxes, such as, for example, sugarcane wax, rice bran wax, or beeswax. Typical commercially available policosanol contains 90% minimum fatty alcohols. The content of individual alcohols vary based on the source of wax and the process of isolation. The fatty alcohols in policosanol are primarily tetracosanol (0.5%-10%), hexacosanol (2%-15%), octacosanol (20%-70%), and triacontanol (5%-20%), while eicosanol, docosanol, heptacosanol, nonacosanol, dotriacontanol, tetratriacontanol, and hexatriacontanol make up the remaining minor constituents.
Policosanol is used as a natural supplement to lower total cholesterol and low-density lipoproteins and raise high-density lipoproteins. Policosanol is a highly lipophilic material, insoluble in water and has poor bioavailability in humans. Policosanol has been reported to reduce cholesterol synthesis in vitro in cell cultures (Singh, D K, Li, L, and Porter, T D, Policosanol inhibits cholesterol synthesis in hepatoma cells by activation of AMP-kinase, J Pharmacol Exp Ther. 2006, 318:1020-6; Menendez R, Amor A M, Rodeiro I, Gonzalez R M, Gonzalez P C, Alfonso J L, Mas R, Policosanol modulates HMG-CoA reductase activity in cultured fibroblasts, Arch Med Res. 2001, 32:8-12). However, in human studies the results have been variable with minimal uptake of policosanol. It has been suggested that the lower and variable efficacy of poilcosanols in human studies can be due to their poor absorption from conventional delivery systems used in the industry. Hence it is desirable to develop an effective delivery system, which is commercially feasible in a cost sensitive supplement industry.